For research use only. Not for therapeutic Use.
Torcetrapib (Cat No.: I002898) is a cholesteryl ester transfer protein (CETP) inhibitor developed to raise high-density lipoprotein (HDL) cholesterol and lower low-density lipoprotein (LDL) cholesterol. It was investigated for cardiovascular disease treatment due to its lipid-modifying effects. Despite promising lipid profile improvements, clinical trials revealed serious adverse effects, including increased blood pressure and cardiovascular risk, leading to its discontinuation. Torcetrapib remains significant in cardiovascular research for understanding CETP inhibition, HDL biology, and the complex relationship between lipid modulation and cardiovascular outcomes in drug development.
| CAS Number | 262352-17-0 |
| Synonyms | ethyl (2R,4S)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-methoxycarbonylamino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinoline-1-carboxylate |
| Molecular Formula | C₂₆H₂₅F₉N₂O₄ |
| Purity | ≥95% |
| Target | CETP |
| Solubility | 10 mM in DMSO |
| Storage | 3 years -20C powder |
| IC50 | 37 nM [1] |
| InChI | InChI=1S/C26H25F9N2O4/c1-4-18-12-21(19-11-15(24(27,28)29)6-7-20(19)37(18)23(39)41-5-2)36(22(38)40-3)13-14-8-16(25(30,31)32)10-17(9-14)26(33,34)35/h6-11,18,21H,4-5,12-13H2,1-3H3/t18-,21+/m1/s1 |
| InChIKey | CMSGWTNRGKRWGS-NQIIRXRSSA-N |
| SMILES | CCC1CC(C2=C(N1C(=O)OCC)C=CC(=C2)C(F)(F)F)N(CC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)C(=O)OC |
| Reference | </br>1:Effects of Torcetrapib and Statin Treatment on ApoC-III and Apoprotein-Defined Lipoprotein Subclasses (from the ILLUMINATE Trial). Bagdade J, Barter P, Quiroga C, Alaupovic P.Am J Cardiol. 2017 Jun 1;119(11):1753-1756. doi: 10.1016/j.amjcard.2017.02.049. Epub 2017 Mar 18. PMID: 28431663 </br>2:Modulating Drug Release and Enhancing the Oral Bioavailability of Torcetrapib with Solid Lipid Dispersion Formulations. Liu Y, Salituro GM, Lee KJ, Bak A, Leung DH.AAPS PharmSciTech. 2015 Oct;16(5):1091-100. doi: 10.1208/s12249-015-0299-8. Epub 2015 Feb 18. PMID: 25690735 Free PMC Article</br>3:In vitro-in vivo evaluation of lipid based formulations of the CETP inhibitors CP-529,414 (torcetrapib) and CP-532,623. McEvoy CL, Trevaskis NL, Edwards GA, Perlman ME, Ambler CM, Mack MC, Brockhurst B, Porter CJ.Eur J Pharm Biopharm. 2014 Nov;88(3):973-85. doi: 10.1016/j.ejpb.2014.08.006. Epub 2014 Aug 23. PMID: 25152213 </br>4:Raising HDL with CETP inhibitor torcetrapib improves glucose homeostasis in dyslipidemic and insulin resistant hamsters. Briand F, Prunet-Marcassus B, Thieblemont Q, Costard C, Muzotte E, Sordello S, Sulpice T.Atherosclerosis. 2014 Apr;233(2):359-62. doi: 10.1016/j.atherosclerosis.2014.01.028. Epub 2014 Jan 23. PMID: 24530763 </br>5:Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility. Kalgutkar AS, Frederick KS, Hatch HL, Ambler CM, Perry DA, Garigipati RS, Chang GC, Lefker BA, Clark RW, Morehouse LA, Francone O, Hu X.Xenobiotica. 2014 Jul;44(7):591-605. doi: 10.3109/00498254.2013.874611. Epub 2013 Dec 31. PMID: 24380613 </br>6:Clarifying off-target effects for torcetrapib using network pharmacology and reverse docking approach. Fan S, Geng Q, Pan Z, Li X, Tie L, Pan Y, Li X.BMC Syst Biol. 2012 Dec 10;6:152. doi: 10.1186/1752-0509-6-152. PMID: 23228038 Free PMC Article</br>7:HDL cholesterol: all hope is not lost after the torcetrapib setback–emerging therapeutic strategies on the horizon. Verma N, Figueredo VM.Am J Ther. 2014 May-Jun;21(3):222-32. doi: 10.1097/MJT.0b013e318249a1b5. Review. PMID: 22967983 </br>8:Relationship between atorvastatin dose and the harm caused by torcetrapib. Barter PJ, Rye KA, Beltangady MS, Ports WC, Duggan WT, Boekholdt SM, DeMicco DA, Kastelein JJ, Shear CL.J Lipid Res. 2012 Nov;53(11):2436-42. doi: 10.1194/jlr.P026328. Epub 2012 Sep 2. PMID: 22941786 Free PMC Article</br>9:Letter by Knop regarding article, /Effect of torcetrapib on glucose, insulin, and hemoglobin A1c in subjects in the investigation of lipid level management to understand its impact in atherosclerotic events (ILLUMINATE) trial/. Knop FK.Circulation. 2012 Mar 6;125(9):e428. doi: 10.1161/CIRCULATIONAHA.111.060152. No abstract available. PMID: 22392871 Free Article</br>10:Letter by McGuire and Aguilar regarding article, /Effect of torcetrapib on glucose, insulin, and hemoglobin A1c in subjects in the investigation of lipid level management to understand its impact in atherosclerotic events (ILLUMINATE) trial/. McGuire DK, Aguilar D.Circulation. 2012 Mar 6;125(9):e427. doi: 10.1161/CIRCULATIONAHA.111.057844. No abstract available. PMID: 22392870 Free Article |
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